cysteine protease inhibitor 2

Cysteine protease inhibitor 2 is a cysteine protease inhibitor. Cysteine protease inhibitor 2 inhibited DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.

Calpain Inhibitor XII (Z-L-Nva-CONH-CH2-2-Py) is a selective and potent inhibitor of calpain I, inhibits calpain II and cathepsin B. Calpain Inhibitor XII shows antiviral activity against coronavirus in cell culture.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

(S)-(+)-Ibuprofen (Dexibuprofen) , is a non-steroidal anti-inflammatory drug (NSAID), inhibiting cyclooxygenase (COX).

2-Cyanopyrimidine (m-Hydroxyphenylpropionic acid) is inhibitor of cathepsin K(IC50 : 170 nM)

Calpeptin is a potent, cell-permeable calpain inhibitor.

Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor (Ki: <20 nM).

Insulin-degrading enzyme (IDE) is a thiol-sensitive zinc-metallopeptidase that acts as the major insulin-degrading protease in vivo, mediating the termination of insulin signaling. [1] In addition to regulating insulin action in diabetes pathogenesis, IDE plays a role in Varicella-Zoster virus infection and degradation of amyloid-β, a peptide implicated in Alzheimer's disease. ML-345 is a small molecule inhibitor that selectively targets cysteine819 in IDE with an EC50 value of 188 nM. [2] It demonstrates 10-fold selectivity for IDE over a panel of enzymes with reactive cysteine residues.[2] Reference:[1]. Maianti, J.P., McFedries, A., Foda, Z.H., et al. Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones. Nature 511(7507), 94-98 (2014).[2]. Bannister, T.D., Wang, H., Abdul-Hay, S.O., et al. ML345, a small-molecule inhibitor of the insulin-degrading enzyme (IDE). 1 R03 DA024888-01 (MLSCN cycle 6), 1-41 (2014).

3CPLro-IN-1 (compound A17) is a potent, orally active inhibitor of SARS-CoV-2 3-Chymotrypsin-like cysteine protease (3CLpro) with an IC50 of 5.65 μM, making it an attractive drug target against COVID-19 and also considered an antitumor agent-51.

SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a highly potent inhibitor specifically designed to target and inhibit the activity of SARS-CoV-2 3CL pro, a cysteine protease found in the main coronaviruses. This enzyme is a promising target for antiviral drug development, positioning SARS-CoV-2 3CLpro-IN-1 as significant for advancing research in infectious diseases [1].

3CPLro-IN-2 is a potent, orally active inhibitor of SARS-CoV-2 3CLpro (IC50: 1.55 μM, Ki: 6.09 μM). 3-Chymotrypsin-like cysteine protease (3CLpro) is an essential protein for viral replication and is a potential drug target against COVID-19.

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K, a cysteine protease expressed under the control of the CTSK gene, which is closely related to osteoporosis and hydrolyses collagen. Cathepsin K inhibitor 2 has shown potential in osteoarthritis.

Z-L(D-Val)G-CHN2, an isoform of Z-LVG-CHN2, serves as a cell-permeable and irreversible inhibitor of cysteine proteinase. This tripeptide derivative emulates a segment of the human cysteine proteinase-binding center and demonstrates selective antiviral activity, inhibiting herpes simplex virus (HSV) yet exhibiting negligible impact on poliovirus replication. Notably, Z-LVG-CHN2 effectively impedes SARS-CoV-2 replication with an EC50 value of 190 nM by targeting the SARS-CoV-2 3CL protease [3].

Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) acts as a cysteine protease inhibitor and has demonstrated efficacy in blocking SARS infection, while also providing protection to mice when challenged with T. crassiceps [1] [2].

PF-00835231 is a CoV-2 cysteine 3C-like protease (3CLpro) inhibitor, with IC50s of 0.27 nM and 4 nM for SARS CoV-2 and SARS CoV-1 3CLpro, respectively. PF-00835231 is the active compound of the first anti-3CLpro regimen in clinical trials.